• Title/Summary/Keyword: Inclusion-complex

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Anti-Proliferative Effects of β-Cyclodextrin Inclusion Complexes with Coumarinolignans from Acer mono (고로쇠 Coumarinolignan의 β-Cyclodextrin 포접화합물 제조 및 암세포증식 억제활성)

  • Yim, Soon-Ho;Jung, Da-Woon;Williams, Darren R.;Geckeler, Kurt E.;Kim, Kyung Keun;Shin, Boo Ahn;Lee, Ik-Soo;Kim, Huyn Jung
    • Korean Journal of Pharmacognosy
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    • v.46 no.2
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    • pp.133-139
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    • 2015
  • Two coumarinolignans, cleomiscosins C (1) and D (2) were isolated from the heartwood of Acer mono, together with four compounds, 5-O-methyl-(E)-resveratrol-3-O-${\beta}$-D-glucopyranoside (3), 5-O-methyl-(E)-resveratrol-3-O-${\beta}$-D-apiofuranosyl-(1$\rightarrow$6)-${\beta}$-D-glucopyranoside (4), scopoletin (5), and (E)-resveratrol-3-O-${\beta}$-D-glucopyranoside (6). Of them, cleomiscosins C (1) and D (2) were applied to preparing inclusion complex molecules with ${\beta}$-cyclodextrin (${\beta}$-CD) to improve the very poor solubility in cell media. The CD complexes of 1 and 2 exhibited an enhancement of water solubility which is feasible to measure their cytotoxicity using a spectrophotometer in a cell-based assay. Anti-proliferative activity of these complex molecules was successfully estimated on HCT116 human colon cancer cells, and cleomiscosin D (2) showed anti-proliferative effects at the concentration of 1.95~31.2 ${{\mu}g}$/mL in a dose-dependent manner.

Effect of Non-Metallic Inclusions and Hot Rolling Process Parameters on Hydrogen Induced Cracking of Linepipe Steels (라인파이프 강재의 수소유기균열에 미치는 열간압연 공정변수의 영향)

  • Koh, Seong Ung;Jung, Hwan Gyo;Kang, Ki Bong
    • Korean Journal of Metals and Materials
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    • v.46 no.4
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    • pp.257-266
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    • 2008
  • AHydrogen induced cracking (HIC) was phenomenologically studied in terms of the effect of nonmetallic inclusions and hot rolling process parameters. By comparing the level of non-metallic inclusions in two different kinds of commercial grade steels having different HIC resistance, the role of non-metallic inclusions in HIC occurrence was investigated. Change in inclusion morphology and distribution during hot rolling was also studied throughout slab, rolling at austenite recrystallization region (roughing mill; RM) and rolling at austenite non-recrystallization region (finish mill; FM). In addition, the contribution of RM and FM parameters to HIC was investigated from the standpoint of change in inclusion morphology during hot rolling processes. As a result, HIC was closely related to the separation of large complex inclusion during hot rolling process. Large complex inclusions originated from the improper Ca treatment, after which equilibrium composition of slag should have resulted in eutectoid composition. By controlling the equilibrium slag composition equivalent to eutectoid one, HIC resistance could be improved due to the reduced size of inclusions. In addition, change in reduction/pass in RM had an effect on HIC resistance of steels while that in FM did not. Increase in the reduction/pass in the latter stage of RM improved HIC resistance of steels by enhancing the void enclosure around inclusions.

Stability Evaluation of Vitamin-C Inclusion Complexes Prepared using Supercritical ASES Process (초임계 ASES 공정으로 제조된 Vitamin-C 포접복합체의 안정성 평가)

  • Yang, Jun-Mo;Kim, Seok-Yun;Han, Ji-Hyun;Jung, In-Il;Ryu, Jong-Hoon;Lim, Gio-Bin
    • KSBB Journal
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    • v.21 no.2
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    • pp.157-163
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    • 2006
  • A supercritical fluid process, called aerosol solvent extraction system(ASES), is especially suitable to the pharmaceutical, cosmetic and food industries due to its environmentally-friendly, non-toxic and residual solvent-free properties. In particular, the application of the ASES process to the processing of thermo-labile bioactive compounds has received attention of many scientists and engineers because of its low-temperature operating conditions. Unstable substances such as Vitamin-C and Vitamin-A can be effectively protected from degradation during the preparation process, because the ASES process is free from oxygen and moisture. In this study, Vitamin-C was formulated with 2-hydroxypropyl-${\beta}$-cyclodextrin (HP-${\beta$-CD) for enhancement of Vitamin-C stability and bioavailability using the ASES process. To investigate the influence of the preparation process on the stability of Vitamin-C, Vitamin-C/HP-${\beta}$-CD inclusion complexes were prepared using both conventional solvent evaporation method and ASES process, and stored in a 50 mM phosphate buffer solution of pH 7.0 at $25^{\circ}C$ for 24 hours. From the experimental results, the stability of the Vitamin-C/HP-${\beta}$-CD inclusion complex prepared from the ASES process was found to be much higher than that of pure Vitamin-C and the Vitamin-C/HP-${\beta}$-CD inclusion complex prepared by the solvent evaporation method. The stability of Vitamin-C was observed to increase with the decrease of temperature at a constant pressure or with the increase of pressure at a constant temperature.

Stress intensity factor and stress distribution near crack tip for infinite body containing regid inclusion with crack shape (균열형상의 강체함유물을 포함하는 무한체에 대한 균열선단 부근의 응력분포와 응력세기계수)

  • Lee, Kang-Young;Kim, Jong-Sung
    • Transactions of the Korean Society of Mechanical Engineers A
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    • v.22 no.3
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    • pp.680-683
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    • 1998
  • In case of the infinite body containing a rigid inclusion with line crack shape, stress intensity factor is determined and the relation between stress intensity factor and stress distribution near a crack tip is developed. Also, the relation between stress intensity factor and Kolosoff stress function is developed. Finally, these results are compared with those that the crack surface is under no traction.

Inclusion Complexation of Cyclodextrin with Prothionamide in Aqueous Solution

  • Kim, Shin-Tae;Kim, Shin-Keun
    • Journal of Pharmaceutical Investigation
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    • v.12 no.4
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    • pp.132-144
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    • 1982
  • The inclusion of ${\beta}-cyclodextrin$ $({\beta}-CyD)$ with prothionamide in aqueous phase was investigated by circular dichroism(CD), ultraviolet (UV) absorption, and solubility technique. The results suggested that a region of drug chromophore was located within the asymmetric center of ${\beta}-cyclodextrin$. Solubility and spectral changes were quantitatively treated to obtain stoichiometric ratio, which was found to be 1 : 1, and formation constants which were determined by solubility, CD, and UV method were 257, 367, and 389 $M^{-1}$, respectively. Also, the formation constant of the inclusion complex was determined by CD method at various pH. The result was that $K_c$ depended upon the pH of medium, and this fact also supported that thioamide moiety was accomodated in the cavity of ${\beta}-cyclodextrin$.

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Physiological Activity of Astaxanthin and its Inclusion Complex with Cyclodextrin (Astaxanthin과 Astaxanthin-Cyclodextrin 포접화합물의 생리활성)

  • Kim, So-Young;Cho, Eun-Ah;Yoo, Gui-Jae;Yoo, Ji-Min;Son, Seok-Min;In, Man-Jin;Kim, Dong-Chung;Chae, Hee-Jeong
    • KSBB Journal
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    • v.24 no.6
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    • pp.570-578
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    • 2009
  • In vitro biological activities such as antioxidant, whitening, anti-hangover and anticancer activities were evaluated. The antioxidant activities of astaxanthin and H. pluvialis extract were significantly higher than that of $\alpha$-tocopherol when the antioxidant activities were determined as xanthine oxidase inhibition, hydroxyl radical scavenging and DPPH radical scavenging. The whitening effect of H. pluvialis extract was about two times as kojic acid. H. pluvialis extract indicated an anticancer activity on a cervical cancer cell line. Astaxanthin showed anti-hangover effect of 1.5 times as jiguja extract. The anti-hangover effect of the inclusion complex (As-$\beta$-CD) was about 1.2 times of jiguja extract. And, the inclusion complex of Haematococcus pluvialis (H.p.-$\beta$-CD) showed almost the same whitening effect as kojic acid.

Improvement in availability and stability of to 106w by inclusion with $\beta-cyclodextrin$ and its derivatives ($\beta-cyclodextrin$ 및 유도체의 포접체 형성에 의한 LG 106W의 유용성 및 안정성 개선에 관한 연구)

  • 정성훈;이천구;조완구;강세훈
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.25 no.1
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    • pp.120-136
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    • 1999
  • A newly synthesized polyhydroxy aromatic compound(LG 106w) has good skin lightening effect. Inclusion complexation of LG 106w with $\beta$-cyclodextrin and its hydroxypropyl and dimethyl derivatives was studied by the solubility method, scanning electron microscopy and differential thermal analysis. A relationship between host and guest was clearly reflected in the magnitude of the stability constant(DM-$\beta$> HP-$\beta$>$\beta$ -cyclodextrin). Formulation problems, which resulted from its very low solubility in aqueous solution, were resolved by the inclusion formation. LG 106W from inclusions is much more water-soluble than pure one. The improvement of pH and temperature stability correlated with the increased solubility was also observed. Inclusion complex of LG 106w had similar activity to pure LG 106w on the inhibition of melanin synthesis in B-16 melanoma cell but showed lower irritation on cultured cell test in vitro. According to the results, cyclodextrins might be one of the reliable candidates for improving the availability of LG 106w.

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Preparation of Microparticulate Itraconazole/Hydroxypropyl-$\beta$-cyclodextrin Inclusion Complexes Using a Supercritical Anti-Solvent [SAS] Process (초임계 역용매 공정을 이용한 Itraconazole/Hydroxypropyl-$\beta$-cyclodextrin 포접복합체 미세입자 제조)

  • 이상윤;김정규;김우식;유종훈;임교빈
    • KSBB Journal
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    • v.19 no.4
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    • pp.321-326
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    • 2004
  • Microparticles of an inclusion complex between itraconazole and 2-hydroxypropyl-${\beta}$-cyclodextrin (HP-${\beta}$-CD) were prepared using an environmentally-benign supercritical anti-solvent (SAS) process. In order to evaluate the degree of complexation, the thermal behavior of solid micro particulate complexes was investigated using differential scanning calorimetry. The experimental results obatined for the solubility and dissolution rate of the microparticulate inclusion complexes in a buffer solution of pH 1.2 showed that the complexation of itraconazole with HP-${\beta}$-CD results in a significant increase in the solubility and dissolution rate of itraconazole. For the microparticulate itraconazole/Hp-${\beta}$-CD inclusion complexes prepared by the SAS process, about 80% of itraconazole was found to dissolve in the buffer solution. Our experimental results confirmed that the SAS process is a promising method for the preparation of microparticles of water-insoluble drug/cyclodextrin inclusion complexes.

Complexation between Venlafaxine Hydrochloride and β -Cyclodextrin:Structural Study by Nuclear Magnetic Resonance Spectroscopy

  • Ali, Syed Mashhood;Koketsu, Mamoru;Asmat, Fahmeena
    • Bulletin of the Korean Chemical Society
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    • v.27 no.9
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    • pp.1397-1400
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    • 2006
  • A detailed spectroscopic study ($^1H$ NMR, COSY, ROESY) of complexation of venlafaxine hydrochloride (VEN) with $\beta$-cyclodextrin ($\beta$--CD) was carried out in solution. The stoichiometry of the complex was determined to be 1 : 1 and penetration of aromatic ring into $\beta$-Cyclodextrin cavity was confirmed from primary rim side, with the help of ROESY spectral data. The structure of the venlafaxine hydrochloride-$\beta$-CD complex has been proposed. The association constant was determined to be 234 $M^{-1}$.

A DPL (DNA/peptide/liposomes) Tripartite Complex Effective for Transfection in Serum

  • Kim Young-Cheol;Park Jong-Gu
    • Biomedical Science Letters
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    • v.10 no.3
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    • pp.187-194
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    • 2004
  • A short peptide corresponding to the nuclear localization signal (NLS) of human immunodeficiency virus (HIV)-l Tat protein, Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg, was employed to improve the efficiency of cellular uptake of nucleic acids. The peptide was first mixed with a reporter plasmid and then with cationic liposomes to form a tripartite complex of DNA/peptide/liposomes (DPL). Transfection efficiency of the DPL complex was compared with that of the conventional DNA/liposomes (DL) complex. When the DPL complex was formed with various cationic liposomes, DOTAP/DOPE (DP) liposome exhibited superior transfection efficiency to other liposomes tested in vitro. With the inclusion of the peptide, the DPL complex showed much enhanced transfection in various cancer cell lines. Particularly, transfection of the DPL complex in serum increased cellular uptake of a transgene up to 2 fold when compared with that in a serum free condition. Further, when the DPL complex was infused through the ureteric route of a rat, transfection efficiency was shown to be better in reporter gene expression than that obtained with the DL complex. This study shows that the DPL complex that is easy to formulate can be employed for much enhanced cellular uptake of a trans gene.

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